Comparative Pharmacology
Head-to-head clinical analysis: MERCAPTOPURINE versus SIKLOS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MERCAPTOPURINE versus SIKLOS.
MERCAPTOPURINE vs SIKLOS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Mercaptopurine is a prodrug that is converted to 6-thioguanine nucleotides, which inhibit de novo purine synthesis and DNA replication by incorporating into DNA and RNA. It also inhibits purine nucleotide interconversions via feedback inhibition of amidophosphoribosyltransferase.
Hydroxyurea inhibits ribonucleotide reductase, reducing the synthesis of deoxyribonucleotides and thereby decreasing DNA synthesis. In sickle cell disease, it increases fetal hemoglobin (HbF) levels, which inhibits sickling of red blood cells.
1.5 to 2.5 mg/kg orally once daily; maintenance 1.5 to 2.5 mg/kg orally once daily.
100–200 mg/kg/day orally in two divided doses, not to exceed 200 mg/kg/day.
None Documented
None Documented
Clinical Note
moderateMercaptopurine + Digoxin
"Mercaptopurine may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateMercaptopurine + Digitoxin
"Mercaptopurine may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateMercaptopurine + Deslanoside
"Mercaptopurine may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateMercaptopurine + Acetyldigitoxin
"Mercaptopurine may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life: 1.5-3 hours (variable); for active metabolites (e.g., 6-thioguanine nucleotides) half-life is 5-7 days, which correlates with myelosuppression.
Terminal elimination half-life is 2-5 hours in adults; shorter in children (1-2 hours). Clinical context: requires thrice-daily dosing to maintain therapeutic concentrations; longer half-life in hepatic impairment (up to 10 hours).
Renal: 20-30% as unchanged drug; biliary/fecal: minor; extensive hepatic metabolism to active and inactive metabolites.
Primarily hepatic metabolism via CYP3A4; renal excretion of metabolites accounts for approximately 70-80% of the dose, with <1% excreted unchanged in urine. Fecal excretion is minor (<5%).
Category D/X
Category C
Antimetabolite
Antimetabolite